Кетофрил®

General characteristics. Structure:

Active ingredient: 30 mg of a ketorolak of a trometamol (a ketorolak of a trometamin) in 1 ml of solution.

Excipients: sodium chloride, dinatrium эдедат, ethanol, water for injections, sodium hydroxide.

Pharmacological properties:

Pharmacodynamics. NPVS derivative of pyrrolizin-carboxyl acid. Has the expressed analgeziruyushchy effect, possesses also antiinflammatory and moderate febrifugal action. The mechanism of action is connected with oppression of activity of TsOG - the main enzyme of metabolism of arachidonic acid, being the predecessor of prostaglandins which play a major role in a pathogeny of an inflammation, pain and fever.

Pharmacokinetics. At intake it is absorbed from a GIT. Cmax in a blood plasma is reached in 40-50 min. both after intake, and after introduction in oil. Meal does not exert impact on absorption. Linkng with proteins of plasma makes more than 99%.

T1/2 is 4-6 h both after intake, and after introduction in oil.

More than 90% of a dose are removed with urine, in not changed look - 60%; other quantity - through intestines.

At patients with renal failures and persons of senile age the speed of removal decreases, T1/2 increases.

Indications to use:

For short-term stopping of moderate and severe pains of various genesis.

Route of administration and doses:

The adult at intake - on 10 mg each 4-6 h, in case of need - on 20 mg of 3-4 times/days.

At introduction in oil a single dose - 10-30 mg, an interval between introductions - 4-6 h. The maximum duration of use - 2 days.

Maximum doses: at intake or introduction in oil - 90 mg/days; for patients with body weight to 50 kg, at renal failures, and also for persons 65 years - 60 mg/days are more senior.

Features of use:

Use at pregnancy and feeding by a breast. It is contraindicated at pregnancy, at the time of delivery and in the period of a lactation (breastfeeding).

Ketorolak is contraindicated for use as means for premedication, the supporting anesthesia and for anesthesia in obstetric practice as under its influence increase in duration of the first period of childbirth is possible. Besides, кеторолак contractility of a uterus and blood circulation of a fruit can oppress.

Use at abnormal liver functions. With care apply at patients with abnormal liver functions.

Use at renal failures. It is contraindicated at the expressed renal failures (content of serumal creatinine more than 50 mg/l), risk of development of a renal failure at a hypovolemia and dehydration.

With care apply at patients with renal failures.

Use for children. It is contraindicated at children's and teenage age up to 16 years.

Use for elderly patients. It is necessary to apply with care кеторолак at patients of senile age since the elimination half-life of a ketorolak is extended, and the plasma clearance can decrease. At these patients it is recommended to apply кеторолак in the doses close to the lower bound of therapeutic range.

Special instructions. With care apply at patients with abnormal liver functions and kidneys, chronic heart failure, arterial hypertension, at patients with erosive cankers of a GIT and bleedings from a GIT in the anamnesis.

It is necessary to apply with care кеторолак in the postoperative period in cases when especially careful hemostasis (including after a prostatectomy, a tonsilectomy, in cosmetic surgery) is required, and also from patients of senile age since the elimination half-life of a ketorolak is extended, and the plasma clearance can decrease. At this category of patients it is recommended to apply кеторолак in the doses close to the lower bound of therapeutic range. At emergence of symptoms of damage of a liver, skin rash, eosinophilia кеторолак it is necessary to cancel. Ketorolak is not shown for use at a chronic pain syndrome.

Influence on ability to driving of motor transport and to control of mechanisms. If during treatment ketorolaky there are a drowsiness, dizziness, sleeplessness or a depression, it is necessary to observe extra care during the occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From cardiovascular system: seldom - bradycardia, changes of the ABP, heartbeat, a syncope.

From the alimentary system: nausea, abdominal pains, diarrhea are possible; seldom - a lock, a meteorism, feeling of overflow of a GIT, vomiting, dryness in a mouth, thirst, stomatitis, gastritis, erosive cankers of a GIT, an abnormal liver function.

From TsNS and peripheral nervous system: the concern, a headache, drowsiness are possible; seldom - paresthesias, a depression, euphoria, sleep disorders, dizziness, change of flavoring feelings, vision disorders, motive disturbances.

From respiratory system: seldom - breath disturbance, suffocation attacks.

From an urinary system: seldom – increase of an urination, an oliguria, a polyuria, a proteinuria, a hamaturia, an azotemia, an acute renal failure.

From system of a blood coagulation: seldom – nasal bleedings, anemia, an eosinophilia, thrombocytopenia, bleedings from postoperative wounds.

From a metabolism: sweating strengthening, hypostases is possible; seldom - an oliguria, increase in level of creatinine and/or urea in a blood plasma, a hypopotassemia, a hyponatremia.

Allergic reactions: the skin itch, hemorrhagic rash are possible; in isolated cases - exfoliative dermatitis, a small tortoiseshell, a Lyell's disease, Stephens-Johnson's syndrome, an acute anaphylaxis, a bronchospasm, a Quincke's edema, mialgiya.

Others: fever is possible.

Local reactions: pain in the place of an injection.

Interaction with other medicines:

At simultaneous use of a ketorolak with other NPVS development of the additive side effects is possible; with pentoksifilliny, anticoagulants (including heparin in low doses) - increase in risk of bleeding is possible; with APF inhibitors - increase in risk of development of renal failures is possible; with probenetsidy - increase concentration of a ketorolak in plasma and the period of its semi-removal; with lithium drugs - decrease in renal clearance of lithium and increase in its concentration in plasma is possible; with furosemide - reduction of its diuretic action.

At use of a ketorolak the need for use of opioid analgetics for the purpose of anesthesia decreases.

Contraindications:

GIT erosive cankers in an aggravation phase, existence or suspicion of gastrointestinal bleeding and/or craniocereberal hemorrhage, disturbances of a blood coagulation in the anamnesis, the states with high risk of bleeding or an incomplete hemostasis, hemorrhagic diathesis moderated and the expressed renal failures (content of serumal creatinine more than 50 mg/l), risk of development of a renal failure at a hypovolemia and dehydration; "an aspirinovy triad", bronchial asthma, nasal cavity polyps, a Quincke's disease in the anamnesis, preventive anesthesia before operation and during operation, children's and teenage age up to 16 years, pregnancy, childbirth, a lactation, hypersensitivity to a ketorolak, acetylsalicylic acid and other NPVS.

Overdose:

Symptoms: vomiting, renal failure, metabolic acidosis, GIT erosive cankers.

Treatment: performing symptomatic therapy (maintenance of the vital functions of an organism). It is not removed sufficiently by means of dialysis.

Storage conditions:

To store at a temperature not above 30 °C in the place protected from light. To store in unavailable to children places. A period of validity - 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 30 mg/ml. 1 ml - ampoules (5) - packagings planimetric plastic (1) - packs cardboard. 1 ml - ampoules (5) - packagings planimetric plastic (2) - packs cardboard.